Alfaxalone: Difference between revisions

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Alfaxalone
Clinical data
AHFS/Drugs.com	International Drug Names
ATC code	N01AX05 (WHO) ;
Legal status
Legal status	US: Schedule IV ;
Pharmacokinetic data
Bioavailability	The alfaxalone molecule is solubilised using SBECD. Cyclodextrins are complex polysaccharides derived from starch that supply a hydrophobic centre for lipophilic drugs like alfaxalone.
Identifiers
	IUPAC name 3α-hydroxy-5α-pregnane-11,20-dione;
CAS Number	23930-19-0 ;
PubChem CID	104845;
ChemSpider	94637 ;
UNII	BD07M97B2A;
KEGG	D07282 ;
ChEMBL	ChEMBL190279 ;
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C21H32O3
Molar mass	332.477 g/mol
3D model (JSmol)	Interactive image;
	SMILES O=C2[C@H]3[C@H]([C@@H]1CC[C@H](C(=O)C)[C@@]1(C)C2)CC[C@H]4C[C@H](O)CC[C@]34C;
	InChI InChI=1S/C21H32O3/c1-12(22)16-6-7-17-15-5-4-13-10-14(23)8-9-20(13,2)19(15)18(24)11-21(16,17)3/h13-17,19,23H,4-11H2,1-3H3/t13-,14+,15-,16+,17-,19+,20-,21+/m0/s1 ; Key:DUHUCHOQIDJXAT-OLVMNOGESA-N ;
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VisualWikitext

Latest revision as of 17:19, 18 August 2015

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Alfaxalone (INN, JAN), also known as alphaxalone or alphaxolone (BAN), is a neuroactive steroid and general anaesthetic.^[1] It is used in veterinary practice under the trade name Alfaxan,^[2] and is licensed for use in both dogs and cats.^{[citation needed]} Along with alfadolone, it is also one of the constituents of anesthetic drug mixture althesin.

Unlike some of its predecessors alfaxalone is not associated with histamine release and anaphylaxis.^{[citation needed]}

A study 1987 found the primary mechanism for the anaesthetic action of alfaxalone to be modulation of neuronal cell membrane chloride ion transport, induced by binding of alfaxalone to GABA_A cell surface receptors. ^[3]

A 1994 study found that alfaxalone binds to a different region of this receptor than the benzodiazepines. .^[4] These benzodiazepine-insensitive GABA_A receptors are located extrasynaptically and are responsible for tonic inhibition. The occurrence of tonic GABA_A inhibition coincides with the expression of relatively rare receptor subunits, particularly the α4, α6, and δ subunits, and as a general rule-of-thumb, δ subunit-containing receptors are extrasynaptic.^[5]

Alfaxalone is metabolised rapidly in the liver. It has a very short plasma elimination half-life in dogs and cats.^{[citation needed]}

References

↑ C.R. Ganellin; David J. Triggle (21 November 1996). Dictionary of Pharmacological Agents. CRC Press. pp. 1094–. ISBN 978-0-412-46630-4.
↑ "Alfaxalone". Drugs.com.
↑ PMID 3819824 (PMID 3819824)
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↑ PMID 7806498 (PMID 7806498)
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↑ Wahab A, Heinemann U, Albus K (October 2009). "Effects of gamma-aminobutyric acid (GABA) agonists and a GABA uptake inhibitor on pharmacoresistant seizure like events in organotypic hippocampal slice cultures". Epilepsy Research 86 (2-3): 113–23. doi:10.1016/j.eplepsyres.2009.05.008. PMID 19535226.

Template:General anesthetics Template:GABAAR PAMs

Template:Nervous-system-drug-stub

[GanellinTriggle1996-1] C.R. Ganellin; David J. Triggle (21 November 1996). Dictionary of Pharmacological Agents. CRC Press. pp. 1094–. ISBN 978-0-412-46630-4.

[2] "Alfaxalone". Drugs.com.

[3] PMID 3819824 (PMID 3819824)
Citation will be completed automatically in a few minutes. Jump the queue or expand by hand

[4] PMID 7806498 (PMID 7806498)
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[5] Wahab A, Heinemann U, Albus K (October 2009). "Effects of gamma-aminobutyric acid (GABA) agonists and a GABA uptake inhibitor on pharmacoresistant seizure like events in organotypic hippocampal slice cultures". Epilepsy Research 86 (2-3): 113–23. doi:10.1016/j.eplepsyres.2009.05.008. PMID 19535226.

[1]

[2]

[3]

[4]

[5]

@@ Line 1: / Line 1: @@
-{{drugbox
+{{Drugbox
-| IUPAC_name        = 3-hydroxypregnane-11,20-dione
+| Verifiedfields = changed
-| image             = Alphaxolone-2D-skeletal.png
+| Watchedfields = changed
-| CAS_number        = 23930-19-0
+| verifiedrevid = 477317167
-| ATC_prefix        = N01
+| IUPAC_name = 3α-hydroxy-5α-pregnane-11,20-dione
-| ATC_suffix        = AX05
+| image = Alfaxalone Wiki Str.png
-| PubChem           = 104845
-| DrugBank          =
+<!--Clinical data-->
-| C=21|H=32|O=3
+| tradename =
-| molecular_weight  = 332.477 g/mol
+| Drugs.com = {{drugs.com|international|alfaxalone}}
-| bioavailability   =
+| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
-| protein_bound     =
+| pregnancy_US = <!-- A / B            / C / D / X -->
-| metabolism        =
+| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 -->
-| elimination_half-life =
+| legal_CA = <!--             / Schedule I, II, III, IV, V, VI, VII, VIII -->
-| excretion         =
+| legal_UK = <!-- GSL         / P       / POM / CD / Class A, B, C -->
-| pregnancy_AU      =  <!-- A / B1 / B2 / B3 / C / D / X -->
+| legal_US = Schedule IV
-| pregnancy_US      =  <!-- A / B            / C / D / X -->
-| pregnancy_category=
+<!--Pharmacokinetic data-->
-| legal_AU          =  <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 -->
+| bioavailability = The alfaxalone molecule is solubilised using SBECD. Cyclodextrins are complex polysaccharides derived from starch that supply a hydrophobic centre for lipophilic drugs like alfaxalone.
-| legal_CA          =  <!--             / Schedule I, II, III, IV, V, VI, VII, VIII -->
-| legal_UK          =  <!-- GSL         / P       / POM / CD / Class A, B, C -->
+<!--Identifiers-->
-| legal_US          =  <!-- OTC                   / Rx-only  / Schedule I, II, III, IV, V -->
+| CAS_number_Ref = {{cascite|changed|??}}
-| legal_status      =
+| CAS_number = 23930-19-0
-| routes_of_administration =
+| ATC_prefix = N01
+| ATC_suffix = AX05
+| PubChem = 104845
+| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
+| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
+| ChemSpiderID = 94637
+| UNII_Ref = {{fdacite|correct|FDA}}
+| UNII = BD07M97B2A
+| KEGG_Ref = {{keggcite|correct|kegg}}
+| KEGG = D07282
+| ChEMBL_Ref = {{ebicite|correct|EBI}}
+| ChEMBL = 190279
+<!--Chemical data-->
+| C=21 | H=32 | O=3
+| molecular_weight = 332.477 g/mol
+| smiles = O=C2[C@H]3[C@H]([C@@H]1CC[C@H](C(=O)C)[C@@]1(C)C2)CC[C@H]4C[C@H](O)CC[C@]34C
+| InChI = 1/C21H32O3/c1-12(22)16-6-7-17-15-5-4-13-10-14(23)8-9-20(13,2)19(15)18(24)11-21(16,17)3/h13-17,19,23H,4-11H2,1-3H3/t13-,14+,15-,16+,17-,19+,20-,21+/m0/s1
+| InChIKey = DUHUCHOQIDJXAT-OLVMNOGEBO
+| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
+| StdInChI = 1S/C21H32O3/c1-12(22)16-6-7-17-15-5-4-13-10-14(23)8-9-20(13,2)19(15)18(24)11-21(16,17)3/h13-17,19,23H,4-11H2,1-3H3/t13-,14+,15-,16+,17-,19+,20-,21+/m0/s1
+| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
+| StdInChIKey = DUHUCHOQIDJXAT-OLVMNOGESA-N
 }}
+__NOTOC__
+{{SI}}
+{{CMG}}
+== Overview ==
+'''Alfaxalone''' ([[International Nonproprietary Name|INN]], [[Japanese Accepted Name|JAN]]), also known as '''alphaxalone''' or '''alphaxolone''' ([[British Approved Name|BAN]]), is a [[neuroactive steroid]] and [[general anaesthetic]].<ref name="GanellinTriggle1996">{{cite book|author1=C.R. Ganellin|author2=David J. Triggle|title=Dictionary of Pharmacological Agents|url=http://books.google.com/books?id=A0THacd46ZsC&pg=PA1094|date=21 November 1996|publisher=CRC Press|isbn=978-0-412-46630-4|pages=1094–}}</ref> It is used in veterinary practice under the trade name '''Alfaxan''',<ref>{{ cite web| url = http://www.drugs.com/international/alfaxalone.html | title     = Alfaxalone| publisher = Drugs.com}}</ref> and is licensed for use in both dogs and cats.{{citation needed|date=November 2011}} Along with [[alfadolone]], it is also one of the constituents of anesthetic [[combination drug|drug mixture]] [[althesin]].
-{{CMG}}
+Unlike some of its predecessors alfaxalone is not associated with histamine release and anaphylaxis.{{citation needed|date=November 2011}}
+A study 1987 found the primary mechanism for the anaesthetic action of alfaxalone to be modulation of neuronal cell membrane chloride ion transport, induced by binding of alfaxalone to [[GABAA|GABA<sub>A</sub>]] cell surface receptors.
+<ref>{{ cite pmid | 3819824 }}</ref>
+A 1994 study found that alfaxalone binds to a different region of this receptor than the [[benzodiazepine]]s.
+.<ref>{{ cite pmid | 7806498 }}</ref> These benzodiazepine-insensitive [[GABAA|GABA<sub>A</sub>]] receptors are located extrasynaptically and are responsible for tonic inhibition. The occurrence of tonic [[GABAA|GABA<sub>A</sub>]] inhibition coincides with the expression of relatively rare receptor subunits, particularly the α4, α6, and δ subunits, and as a general rule-of-thumb, δ subunit-containing receptors are extrasynaptic.<ref>Wahab A, Heinemann U, Albus K (October 2009). "Effects of gamma-aminobutyric acid (GABA) agonists and a GABA uptake inhibitor on pharmacoresistant seizure like events in organotypic hippocampal slice cultures". Epilepsy Research 86 (2-3): 113–23. doi:10.1016/j.eplepsyres.2009.05.008. PMID 19535226.</ref>
+Alfaxalone is metabolised rapidly in the liver. It has a very short plasma elimination half-life in dogs and cats.{{citation needed|date=November 2011}}
+==See also==
+* [[Ganaxolone]]
+* [[Hydroxydione]]
+* [[Minaxolone]]
+* [[Pregnanolone]]
+* [[Renanolone]]
+==References==
+{{Reflist|2}}
-'''Alfaxalone''' ([[International Nonproprietary Name|INN]], also known as '''alphaxalone''' or '''alphaxolone''') is a [[steroid]]al [[general anaesthetic]]. It is one of the constituents of [[althesin]].
 {{General anesthetics}}
+{{GABAAR PAMs}}
+{{Glycinergics}}
+[[Category:Drug]]
+[[Category:General anesthetics]]
+[[Category:Neurosteroids]]
+[[Category:Alcohols]]
+[[Category:Ketones]]
+[[Category:GABAA receptor positive allosteric modulators]]
+[[Category:Glycine receptor agonists]]
-{{WH}}
+{{nervous-system-drug-stub}}
-{{WS}}

Alfaxalone: Difference between revisions

Latest revision as of 17:19, 18 August 2015

Overview

See also

References

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